Taxonomic Class

Piperaceae

Common Trade Names

Aigin, Antares, Ardeydystin, Cetkava, Kava Kava Liquid, Kava Kava Root, Kavarouse, Kavasedon, Kavasporal, Kava Stress, Kavatino, Kavatrol, laitan, Mosaro, Nervonocton N, Potter’s Antigian Tablets, Super 5HT with Kava, Viocava

Common Forms

Prepared as capsules, a drink from pulverized roots, an extract, or tablets. Source

Kava comes from the dried rhizome and root of Piper methysticum, a member of the black pepper family (Piperaceae). Kava, a large shrub with broad, heart-shaped leaves, is native to many South Pacific islands.

Chemical Components

Pharmacologic activity is attributed to the kavapyrones that occur in the root. Biologically active components are obtained from chemical substitution of the basic pyrone structure. Alpha-pyrone components include yangonin, desmethoxyyangonin, 5,6-dehydromethysticin, ll-methoxyyangonin, and] 1-methoxy-nor-yangonin. Methysticin, kawain, dihydromethysticin, and dihydrokawain are active components from the 5,6-dyhydro-alpha-pyrone structure. Pipermethystine is an alkaloid isolated from the plant leaves of kava.

Actions

More than one mode of action is involved. An unquantified synergism exists among kava components. Components of the root may produce local anesthetic activity similar to that of cocaine but lasting longer than that of benzocaine. Kava induced mephenesin-like muscle relaxation in animals but was found to lack curare-like activity. The limbic system is inhibited by kavapyrones, an effect associated with suppression of emotional excitability and mood enhancement. Kava also inhibited haloperidol-induced catalepsy in rats .

In human studies, kava produced mild euphoria with no effects on thought and memory. The neuropharmacologic effects of kava include analgesia, hyporeflexia, and sedation. Kava can impair gait and cause pupil dilation. Some pyrones show fungistatic properties against several fungi, including some that are pathogenic to humans.

Reported Uses

Kava has been useful in attenuating spinal seizures and has antipsychotic properties. Therapeutic trials have shown a degree of seizure control in epileptic patients, suggesting involvement of gamma-aminobutyric acid receptors.

Kava extract has also been studied for treating anxiety disorders. In one study, 101 patients with anxiety of nonpsychotic origin showed improved scores on the Hamilton Anxiety Scale after being given a lipophilic extract of kava standardized to 70 mg of kavalactones three times a day . Both placebo and kava showed benefit as per the scale after 8 weeks, but kava fared significantly better than placebo at 16 weeks (P<.0001). No improvement was seen as measured on the Clinical Global Impression Scale. A meta-analysis of seven double­blind, randomized, placebo-controlled trials found some superiority of kava over placebo for treating anxiety in all trials but statistically significant superiority in only three trials .

Other claims for kava include treatment of asthma, depression, insomnia, muscle spasms, pain, rheumatism, and sexually transmitted disease and promotion of wound healing.

Dosage

Dosage is usually based on the kavapyrone content, which varies with preparation. Most studies in humans used 70 to 240 mg of kavapyrone P.O. daily. One study used 90 to 110 mg of dried kava extract P.O. t.i.d. for the treatment of anxiety . Doses of freshly prepared kava beverages average 400 to 900 g P.O. weekly.

Adverse Reactions

CNS: changes in motor reflexes and judgment, headache, dizziness.

EENT: vision changes.

Long-term, heavy use

CV: hypertension.

GI: diarrhea.

Hematologic: decreased platelet and lymphocyte counts.

Metabolic: reduced plasma protein, urea, and bilirubin levels; weight loss.

Musculoskeletal: increased patellar reflexes.

Respiratory: shortness of breath.

Skin: hypersensitivity reaction .

Other: dopamine antagonism (potential for galactorrhea and breast engorgement), reddened eyes and dry, flaking, discolored skin.

Interactions

Alcohol: Increased kava toxicity. Avoid administration with kava.

Alprazolam: May cause coma . Avoid administration with kava.

Benzodiazepines, other CNS depressants: Additive sedative effects. Avoid administration with kava.

Levodopa: Increased parkinsonian symptoms. Avoid administration with kava.

Pentobarbital: May have additive effects. Avoid administration with kava.

Contraindications And Precautions

Avoid using kava in pregnant or breast-feeding patients and in children under age 12; effects are unknown. Use cautiously in patients with neutropenia, renal disease, or thrombocytopenia. Avoid administration with psychotropic drugs.

Special Considerations

Inform the patient that significant adverse reactions may occur with long-term use of kava.

Caution the patient to avoid alcohol and other CNS depressants because they enhance kava’s sedative and toxic effects.

Inform the patient that absorption of kava may be enhanced if it is taken with food.

Advise women to avoid taking kava during pregnancy or when breast­feeding.

Points of Interest

Kava, although a depressant, is non fermented, nonalcoholic, nonopioid, and nonhallucinogenic and does not appear to cause physiologic dependence, but the risk of psychological dependence exists.

Kava is commonly used in the South Pacific as a ceremonial beverage.

Commentary

Kava has been used or studied most commonly for the treatment of ahxiety, restlessness, and stress. These uses are supported by limited evidence from a few small clinical trials. In studies of kava as an anxiolytic, adverse reactions were minimal, but significant adverse reactions are re­ported with chronic, heavy use. Other therapeutic claims are poorly documented. Additional trials are needed to establish dosing regimens, drug interactions, therapeutic benefits, and adverse effects.

Taxonomic Class

Juglandaceae

Common Trade Names

None known.

Common Forms

Available as a decoction, an extract, and a tincture and used externally as a bath additive and a compress.

Source

The leaves of the deciduous tree (Juglans regia), the bark, the hull of the nut, and the nut itself have been used for various preparations.

Chemical Components

The leaves contain about 10% tannins of the ellagitannin type; naphthalene derivatives, especially the monoglucosides of juglone (=5- hydroxy-1,4-naphtholquinone) and hydrojuglone; more than 3% flavonoids (such as quercetin, quercitrin, hyperoside, and kaempferol derivatives); 0.8% to 1% ascorbic acid, plant acids, including gallic, caffeic, and neochlorogenic acids; and 0.001 % to 0.03% volatile oil, mainly germacrene D. The main active components are the tannins and juglone.

Actions

J. regia is mainly used externally as an astringent, based on its tannin content (10%). Juglone and the essential oils may have in vitro antifungal activity and, possibly, antitumorigenic effects in mice. The actual nut has been studied as a substitute (replacing 20% to 35% of monounsaturated fat foods) in cholesterol-lowering diets with success in further reducing total cholesterol and LDL levels in human subjects .

Reported Uses

Walnut preparations have been used externally for acne, eczema, eyelid inflammation, excessive perspiration of the hands and feet, pyodermia, tuberculosis, and various skin ulcers. It has been used internally for catarrhs of the GI tract and as an anthelmintic and a blood-purifying agent.

Dosage

Dosing is highly dependent on various factors. Because no standard production exists, dosage ranges must be viewed as relative guidelines.

External: 3 to 6 g/day; 100 g per full bath.

Extracts: 2 to 3 g P.O. once to several times a day.

Tincture: 1 to 3 ml P.O. once to several times a day.

Adverse Reactions

Hepatic: hepatotoxicity (caused by tannin content).

Other: carcinogenic effects (potential with long-term use of J. regia as an external preparation).

Interactions

None reported.

Contraindications and Precautions

Excessive oral ingestion and topical application of walnuts should be avoided in pregnant or breast-feeding patients.

Special Considerations

• Caution the patient who is at risk for heptatotoxicity about ingesting considerable quantities of walnut because the tannin content may increase the risk of hepatic injury.
• Advise the patient who is looking for a natural agent to reduce serum cholesterol levels to pursue more stringently studied and proven alternatives.
• Inform the patient that walnut preparations that contain juglone compounds can discolor the skin or mucous membranes yellowish brown.
• Caution the patient that daily topical application of walnut preparations may increase the risk of tongue cancer and leukoplakia of the lips.

Commentary

Little, if any, evidence exists other than in vitro studies to support most of the claims for the use of walnut. Larger human trials are needed to demonstrate its effectiveness in hypercholesterolemic men and Women. More research is needed before definitive recommendations can be put forward.

Taxonomic class

Smilacaceae

Common Trade Names

Multi-ingredient preparations: Sarsaparilla, Sarsaparilla Root Extract

Common Forms

Available as capsules (425 mg, 520 mg), dried root powder, liquid (30 ml), solid root extract, tablets, and teas.

Source

The dried roots and rhizomes of various Smilax species (S. aristochiifolia, S. regelii, S. febrifuga, S. ornata) are used in commercial products. Smilax species are cultivated in Mexico, Jamaica, and South America.

Chemical Components

Saponins constitute] % to 3% of the chemical components of sarsaparilla, with the three main saponins being sarsaponin (parillin), smilasaponin (smilacin), and sarsaparilloside. Other saponins include sarsapogenin (parigenin), smilagenin, diosgenin, tigogenin, aspergenin, and laxogenin. Phytosterols, such as beta-sitosterol, may contribute to an anti-inflammatory effect. Resins, starch, trace volatile oils, and cetyl alcohol constitute the remainder of the compound.

Actions

Sarsaparilla’s pharmacologic effects have been attributed to the saponins, which are claimed to be blood purifiers or tonics that supposedly remove unwanted toxins from the body. This idea might have arisen from sarsaparilla’s supposed diaphoretic and diuretic effects. Other purported effects of saponins include an ability to bind serum cholesterol in the GI tract and a hemolytic effect if administered IV These pharmacologic effects are not well documented.

Sarsaparilla has shown in vitro activity against common dermatophytes . Significant anti-inflammatory activity and prevention of chemically induced hepatocellular damage have been noted in rodents . Sarsaparilla was found not to have any beneficial effects for improving the healing of bone fractures in rats.

Reported Uses

Sarsaparilla root is claimed to be useful for treating renal disease, rheumatism, and skin diseases such as psoriasis and eczema. Older research attempts to substantiate sarsaparilla for use in psoriatic disease.

The most notable trial involved patients with psoriasis vulgaris who received sarsaponin (a major component of sarsaparilla) or placebo . Although the study showed favorable results in terms of improved symptoms, duration of benefit, and reduced disease exacerbations, problems with study design led to questions regarding the final conclusions reached.

Because of its steroidal components, sarsaparilla has also been touted as an athletic performance-enhancing agent. These steroids have not been proven to be anabolic, and therefore, this claim remains unsubstantiated. Sarsaparilla has been promoted as an appetite and digestion aid and as a diuretic. Its extract has been evaluated as adjunctive therapy in leprosy .

The 1992 German Commission E monograph advocates the use of sarsaparilla in treating psoriasis, renal disease, and rheumatic complaints and for diaphoresis and diuresis.

Sarsaparilla is accepted by the FDA as a flavoring agent.

Dosage

For psoriasis, 1 to 4 g of dried root, 8 to 30 ml of concentrated sarsaparilla compound decoction, or 8 to 15 ml of liquid extract P.O. t.i.d. has been suggested.

Adverse Reactions

CV: hypotension.

GI: diarrhea, GI irritation.

GU: renal dysfunction.

Hematologic: hemolysis (I.V. use).

Metabolic: electrolyte imbalances.

Respiratory: asthma (inhalation of root dust).

Interactions

Bismuth: May increase absorption or elimination or both. Avoid administration with sarsaparilla.

Certain hypnotic drugs: Increased elimination. Monitor for lack of effectiveness.

Digitalis: Increased absorption. Do not use together.

Oral drugs: Saponins may affect absorption of other drugs. Other drugs should be taken 2 hours before or after taking sarsaparilla.

Contraindications and Precautions

Avoid using sarsaparilla in pregnant or breast-feeding patients; effects are unknown.

Special Considerations

• Inform the patient that therapeutic claims for sarsaparilla are weakly substantiated.
• Advise the patient with asthma to avoid inhaling sarsaparilla root dust or root particles.
• Caution the patient who is already taking a diuretic about excessive diuretic effects, fluid and electrolyte imbalances, and hypotension.

Points of Interest

• Since the] 6th century, sarsaparilla was thought to be an effective treatment for syphilis. It gained popularity in the Old West of the United States and was the drink of choice for cowboys. It was even listed for such uses in the USP from 1820 to 1910. Activity against syphilis has not been pharmacologically substantiated.

Commentary

The use of sarsaparilla for any condition needs further research. Mechanisms and properties are not clearly documented or adequately researched. The most notable clinical trial evaluated the herb’s use in study design and the presence of confounding variables placed the conclusions in question.

Taxonomic class

Rosaceae

Comman Trade Name

None known

Common forms

Available as decoctum cydoniae, B.P. (decoction from seeds), fruit syrup, and mucilage of quince seeds.

Source

The fruit and seeds of Cydonia oblonga are used in preparing the medicinal products of quince.

Chemical Components

The seeds contain fixed oil, protein, and a small amount of amygdalin, and its coat contains mucilage. The fruit pulp contains malic acid. Beta­D- glucopyranosyl-(1,6) -beta -D-glncopyranoside of 3- hydroxy-beta­ionol has also been isolated in the fruit.

Actions

Tertiary literature suggests astringent, cardiac, demulcent, diuretic, emollient, and restorative effects. A decoction of C. Oblonga has been shown in vitro to have a bactericidal effect against Vibrio cholerae .

A German abstract describes a three-way crossover study examining varying strengths of a mixture of extracts from both Citrus limon and C. oblonga and their effects on nasal mucociliary clearance . The investigators failed to detect a change in nasal mucociliary clearance.

Reported Uses

Traditionally, quince fruit syrup has been commonly added to beverages to treat diarrhea, dysentery, and sore throat. The decoction from the seeds is taken internally in the treatment of dysentery, gonorrhea, and thrush; it is also used as an adjunct in boric acid eye lotions and in skin lotions and creams. Anecdotal data exist for these uses; no clinical human data are available. The mucilage of quince seeds has been used as a suspending agent in such pharmaceutical and toilet preparations as mouthwashes for canker sores, gum problems, and sore throats. Although the quince seeds are thought to be useful in treating cancer probably because of amygdalin’s cyanogenetic action-no studies have confirmed this effect.

Dosage

For diarrhea, dysentery, gonorrhea, and thrush, large quantities of decoctum cydoniae (2 drams of quince seed boiled in 1 pt of water for 10 minutes) P.O.

No dosages have been reported for the external use of mucilage preparations.

Adverse Reactions

None reported .

Interactions

None reported.

Contraindications and Precautions

Avoid using quince in pregnant or breast-feeding patients; effects are ,known.

Speciacial Considerations

• Advise the patient taking quince for GI symptoms that other agents with known safety and efficacy data are available.

Alert Quince seeds are potentially toxic because of their amygdalin (laetrile) content.

• Caution the patient to keep quince out of the reach of children and pets.

Points of Interest

• Other varieties of quinces, especially the Japanese quince, Cydonia illponica, are not used medicinally.
• Japanese quince is a popular ornamental plant that is grown all over the world.

Commentary

Preparations made from the fruit or the mucilage derived from the seed (oat may provide minor relief from diarrhea and sore throat because of their astringent and demulcent properties. Although a quince decoction has been shown to have an in vitro bactericidal effect against V. cholerae there are no clinical reports suggesting its value in treating cholera. The amygdalin (laetrile) component of quince is toxic and ineffective as a cancer treatment and should not be consumed.

Common Trade Names

Biodynamic Lemon Balm Liquid Herbal Extract.

Common Forms

Lemon balm (Melissa officinalis L.) is usually taken as a tea made from either dried or fresh leaves. Liquid extracts are available. Preparation of a poultice has also been reported in the lay literature and a formulated cream has been used in some clinical trials.

Source

M. officinalis is a member of the mint family. Active chemical constituents can be found in the leaves and stems. The leaves are opposite, ovate, bluntly serrate, and acuminate. The flowers are bilabiate and range in color from white to light blue.

Chemical components

Numerous compounds have been isolated from lemon balm, including caffeic acid, citral, citronellal, eugenol, geraniol, choline, and an unidentified glycoside.

Actions

The efficacy of eugenol in dental analgesia is well established, and it is probably this component that accounts for the usefulness of lemon balm in toothache. Aqueous methanoJic extracts have demonstrated a concentration-dependent inhibition of lipid peroxidation. Early scientific data reported possible antibacterial and antiviral properties of lemon balm. These reports have been supported by data that indicates potent activity against HIV-1 by aqueous extracts . In vitro studies have also demonstrated antiprotozoal activity against Trypanosoma brucei specificially . Additional research has indicated that certain constituents of the plant (caffeic acid and an unidentified glycoside) inhibit protein synthesis by direct interference with elongation factor 2. Numerous studies by various laboratories have supported these data. This may account for the antiviral activity of the herb. Ethanolic extracts have demonstrated an affinity for cholinergic receptors in human cerebral cortical tissue. This affinity was predominantly for nicotinic receptors with less but significant affinity for muscarinic receptors . Clinical trials of lemon balm cream for local treatment of herpes labialis demonstrated significant improvement in time to heal, spread of lesions, and attenuation of symptoms relative to placebo control . No animal or human studies exist to establish the toxicity of lemon balm.

Reported Uses

Nonmedical uses of lemon balm include its use in potpourri, herb pillows, and cosmetics and as a garnish or herb in cooking. The lay literature touts numerous therapeutic benefits for lemon balm, including its use as an antiflatulent, an antipyretic, an antispasmodic, a carminative, an emmenagogue, a sedative, a stomachic, and a sudorific. It has also been used by herbalists as a treatment for asthma, chronic bronchial catarrh, headache and vertigo in pregnancy, hysteria, melancholy, migraine headache, and toothache. Other uses purported for lemon balm as a poultice for local treatment of wounds, tumors, and insect bites; I,) relieve menstrual cramps; and in the treatment of herpes simplex lesions. Proposed cholinergic activity has led to lemon balm’s being suggested as an alternative therapy for various derangements of memory, IIlduding Alzheimer’s disease . No data exist that establish the extent of use of lemon balm by the public.

Dosage

I ,emon balm is most often taken as a tea, prepared from either fresh or dried leaves. The tea is prepared by steeping a bag of leaves (1 tsp) for about 5 minutes in hot water. Sometimes a stronger tea is made by placing 1,1/2 tbsp of the leaves in1 pt of boiling water, covering it, and steeping it for 15 minutes before straining. Dosage for the liquid extract is recommended to be 2 to 4 ml P.O, t.i.d.

Adverse Reactions

Skin: local irritation.

Other: hypersensitivity reactions.

Interactions

None reported.

Contraindications and precautions

No contraindications or precautions have been reported for lemon balm. One study that examined the ability of different antiviral compounds used in the treatment of herpes simplex to evoke a sensitivity reaction reported that an extract of lemon balm induced a weak response (less than the antiviral tromantadine) in guinea pigs. People who have a propensity to develop allergic reactions should use the herb cautiously. A second study examined the mutagenic properties of several medicinal plants, using an Aspergillus nidulans plate incorporation assay as the model. No mutagenic or genotoxic effects were noted for either aqueous or alcoholic extracts of lemon balm. No other studies using more stringent models of mutagenicity, teratogenicity, or genotoxicity exist. Given the ability of caffeic acid and the glycoside to inhibit protein synthesis, the use of lemon balm in pregnancy should be strongly discouraged, despite its purported efficacy in treating gravidal headache and dizziness.

Special considerations

Caution the patient who is prone to allergic reactions to avoid using lemon balm.

Advise pregnant patients to avoid using lemon balm.

Advise the patient to consult a health care provider before using herbal preparations because a treatment that has been clinically researched and proved effective may be available.

Although no known chemical interactions have been reported in clinical studies, consideration must be given to the pharmacologic properties of the herbal product and the potential for exacerbation of the intended therapeutic effect of conventional drugs.

Commentary

Potential benefit may be possible when lemon balm is used as recommended. A few scientific studies do support the possible efficacy of certain constituents as an anti-inflammatory and a memory aid. No clinical studies support these uses nor has the toxicological profile of these actions been determined.

The widespread use of lemon balm in cooking implies that it is probably safe when ingested in small amounts. Most information concerning its medical uses comes from the lay literature and does not constitute a valid recommendation for its use. Extensive scientific research is needed to provide a basis for the use of caffeic acid, the glycoside, or some derivative of these chemicals as an antiviral. Also, controlled scientific and clinical studies are needed to establish safe therapeutic doses and adverse effect and toxicity profiles of lemon balm.

Common Trade Names

None known.

Common Forms

Available as capsules and powder and in beverages and other herbal formulas.

Source

Vanadium is a trace mineral that is found in the earth’s crust and in rocks, some iron ores, and crude petroleum deposite. In nature, it is often found as crystals. It usually combines with other elements such as oxygen, sodium, sulfur, and chloride.

Chemical Components

Vanadium is found combined with other elements and particles in soil and in low levels in plants.

Actions

Vanadium is an antioxidant that may playa role in the mineralization of bones and teeth. Animal studies have also suggested that vanadium may improve insulin action or mimic insulin in rats . These studies also imply that vanadium may inhibit cholesterol synthesis. The amount of vanadium needed to mimic insulin was high, to the point of toxicity, causing poor appetite and growth, diarrhea, and death in many of the animals.

Reported Uses

Therapeutic claims for vanadium include its use as a muscle, strength, or performance enhancer and as a supplement to improve glucose metabolism and to treat and prevent diabetes and high cholesterol levels. These claims have not been supported by human trials and are based on animal trials in which high doses were used that produced toxic symptoms. Deficiency symptoms have not yet been identified in humans and even the most nutritionally inadequate diet has been shown to contain sufficient quantities to prevent deficiency .

Dosage

No RDA has been established. Estimated requirements for adults are 1 to 3 mcg/day P.O. with dietary intake usually 10 to 60 mcg. Available dosage forms supply a wide range of dosage strengths (1-100 mg).

Adverse Reactions

ENS: confusion.

EENT: eye inflammation, green tongue.

GI: anorexia, diarrhea.

Hematologic: anemia.

Respiratory: cough, pleurisy, wheezing.

Musculoskeletal: growth retardation.

Other: death.

Interactions

Chromium and vanadium: May interfere with each other’s absorption. Separate administration times.

Smoking: Decreased vanadium absorption. Avoid smoking when taking this herb.

Contraindications and Precautions

Vanadium is contraindicated in pregnant patients; birth defects were reported in animal studies.

Special Considerations

• Caution the patient against using vanadium because little evidence regarding its medicinal use exists.
• Advise the patient to consult a health care provider before using herbal preparations because a treatment that has been clinically researched and proved effective may be available.
• Monitor for adverse reactions in patients who are taking more than 10 mcg/day.
• Advise the female patient to report planned or suspected pregnancy.

Commentary

Insufficient data exist in humans to support any medicinal use of vanadium. Animal studies have produced some insulin-like effects but at doses that are known to be toxic. The danger of toxicity warrants that this supplement not be recommended.

Taxonomic class

Cactaceae

Common Trade Names

Multi-ingredient preparations: Cactus Grandiflorus, Cactus-Hawthorn

Compound, Cereus Grandiflorus, Night-Blooming Cereus

Common Forms

Available as liquid extract and tincture.

Source

Active components are derived from the stems and flowers of Selenicereus grandiflorus, which is native to tropical and subtropical America , including the West Indies .

Chemical Components

The plant contains a digitalis-like glycoside, either cactine or hordenine (N,N -dimethyl -4- hydroxy-beta - phenethylamine). Other reported components include betacyanin, isorhamnetin-3-glucoside, narcissin, rutin, cacticine, kaempferitrin, grandiflorine, hyperoside, isorhamnetin-3-beta­galactosyl- rutinoside, and isorhamnetin- 3-beta- xylosyl- rutinoside.

Actions

Night-blooming cereus is thought to elevate arteriolar tension by increasing the muscular energy of the heart and causing arteriolar contraction. This theory has not been confirmed by human data. Early research with commercial preparations of the active compound proved it to be physiologically inert. More recently, in studies with rats and dogs, hordenine showed a positive inotropic effect on the heart, with increased systolic and diastolic blood pressures and peripheral blood flow volume . Flavonoids and their derivatives (rutin, rutinoside, and kaempferitrin) are thought to improve capillary function by decreasing abnormal leakage .

Reported Uses

In Europe , the liquid plant extract has been used to treat angina pectoris, irritable bladder, kidney congestion, nervous headache, palpitations, and prostatic diseases. The herb has been used as an antirheumatic and a cardiotonic in Cuba . Other indications for its use include cystitis, dyspnea, edema, endocarditis, and myocarditis. Anecdotal reports claim that the herb is valuable as a cardiac stimulant and a partial substitute for digitalis in heart disorders related to anemia, dyspepsia, Graves’ disease, neurasthenia, and tobacco toxicity.

Dosage

Traditional uses suggest the following dosages:

Liquid extract: 0.7 ml (12 minims) P.O. every 4 hours.

Tincture: 1 to 1.8 ml (15 to 30 minims) P.O. every 4 hours.

Adverse Reactions

EENT: burning sensation in the mouth.

GI: diarrhea, nausea, vomiting.

Interactions

ACE inhibitors, antiarrhythmics, beta blockers, calcium channel blockers, cardiac glycosides: May increase effects of these drugs. Avoid administration with night-blooming cereus.

Contraindications and Precautions

Night-blooming cereus is contraindicated during the first trimester of pregnancy.

Special Considerations

Monitor the patient’s heart rate and blood pressure if the is also taking prescription cardiac drugs.

Encourage the patient with a CV disorder to be evaluated by a health care provider and, if necessary, receive prescribed cardiac drugs. Because the use of night-blooming cereus as a substitute for digitalis has not been confirmed by human clinical trials, it should not be used by itself for heart-related disorders.

Urge the patient to immediately report heart-related adverse effects (blood pressure changes, increased heart rate, and palpitations) to his health care provider.

Instruct women to report planned or suspected pregnancy.

Advise women to avoid using night-blooming cereus during pregnancy or when breast-feeding.

Commentary

Although night-blooming cereus contains a digitalis-like glycoside, its use as a substitute for digitalis preparations (digoxin or digitoxin) or for treating heart-related disorders has not been evaluated in humans. Patients with such conditions should strongly be encouraged to seek professional medical advice. Also, patients who are taking prescription digitalis or other cardiac drugs should avoid concurrent use of this herb.

Taxonomic class

Caricaceae

Common Trade Names

Papaya Enzyme, Papaya Enzyme with Chlorophyll, Papaya Leaf

Common Forms

Tablets: 5 mg

Tablets (chewable): 25 mg

Also available as a tea.

Source

Components are usually extracted from the leaves, seeds, pulp, and latex of Carica papaya, which is native to Mexico and Central America but also grows in other tropical areas.

Chemical Components

Papaya is composed primarily of proteolytic enzymes, including papain and chymopapain. Papain (also know as vegetable pepsin) occurs in the leaves and fruit latex. The alkaloid carpaine has also been isolated from the leaves. The seeds contain the glycosides caricin and myrosin.

Actions

Meat, seeds, and plant pulp of unripe papaya have demonstrated antioxidant properties and exerted weak bacteriostatic activity in vitro.

Latex from papaya sap has inhibited the growth of Candida albicans in culture .

Reported Uses

Papain is classified as a debriding agent for necrotic tissue. Chymopapain is approved for intradiskal injection in patients with herniated lumbar intervertebral disks who do not respond to conventional therapy.

Papaya was used for athletic injuries and showed improved anti­inflammatory response and speedy recovery . It was also helpful in reducing postoperative edema and ecchymosis after nasal plastic surgery. In patients who had undergone head and neck surgery, papaya reduced postoperative edema slightly .

Papain is claimed to be useful as an anthelmintic and in treating digestive disorders. The latex has been effective against intestinal nematodes in mice.

Dosage

For inflammation, clinical trials suggest 10 mg P.O. q.i.d. for 7 days.

Adverse Reactions

CNS: decreased CNS activity (carpaine), paralysis.

CV: decreased heart rate.

GI: perforation of the esophagus and severe gastritis (with ingestion of excessive papaya or papain).

Skin: carotenemia, dermatitis.

Other: anaphylactic shock (reported after injection of chymopapain), hypersensitivity reactions (plant parts, extracts).

Interactions

None reported.

Contraindications and Precautions

Avoid using papaya in pregnant or breast-feeding patients; effects are unknown. Use cautiously in patients with a history of atopy or in those who are prone to contact dermatitis reactions from the herb.

Special Considerations

Monitor the patient with hypersensitivity for reactions to papaya.

Caution the patient against prolonged use because of the risk of severe gastritis and hypersensitivity reactions. Explain that the latex in the plant may induce dermatitis.

Advise Women to avoid using papaya during pregnancy or when breast -feeding.

Points of Interest

Papaya is a source of flavoring used in candies and ice cream.

Papain is used in Some facial creams to soften skin and as a meat tenderizer.

Commentary

Human clinical trials suggest that papaya may be useful in treating inflamation caused by trauma or surgical procedures. In vitro studies have documented bacteriostatic effects against enteropathogens, but human clinical trials need to be conducted to verify these claims. Because allergic reactions have been caused by plant parts and extracts, papaya should be used cautiously in patients with a history of hypersensitivity reactions.

Taxonomic class

Rosaceae

Common Trade Names

Alvita Teas Hawthorne Berry, Cardio Health Hawthorne Berry #6 Syrup, Cardiplant, Gaia Herbs Hawthorn Berry A/F, Gaia Herbs Hawthorn Berry Solid, Gaia Herbs Hawthorn Supreme, Gaia Herbs Hawthorn Supreme SFSE, Hawthorne Berry, Hawthorne Formula, Hawthorne Heart, Hawthorne Phytosome, Hawthorne Power, Heart Foods Company Hawthorne plus, Heart Foods Company Power Caps Hot Cayenne with Hawthorne and Ginger, Herbalist and Alchemist Hawthorn-Cactus Extract, Herbalist and Alchemist Hawthorn­Fruit/Flower Extrac, Natrol Hawthorne Berry Capsules, Nature’s Answer Hawthorne Berry Low Alcohol, Nature’s Answer Hawthorne C+ Combo, Standardized Full Potency Hawthorne Berry Extract Vegicaps

Common Forms

Available as biological extracts (4 mg/ml of vitexin-2-0-rhamnoside); capsules of berries (510 mg) or leaves (80 mg) standardized to 15 mg of oligomeric procyanidines; and extended-release capsules (300 mg of 1.8% vitexin-2-rhamnoside and hyperoside).

Source

Active ingredients are extracted from the berries, flowers, and leaves of

Crataegus species, commonly C. laevigata, C. monogyna, or C. folium. More than 300 Crataegus species are found in the temperate regions of North America, Asia, and Europe.

Chemical components

Hawthorn is composed primarily of proanthocyanidins and flavonoids (quercetin, hyperoside, vitexin, vitexinrhamnoside, rutin); other constituents include catechin and epicatechin.

Actions

Studies on animals and in vitro models have suggested CV actions that

include ACE inhibition, beta-blocking activity, dilation of coronary arteries, hypotensive effects, and negative and positive inotropic effects. The high bioflavonoid content in some hawthorn species may show antioxidant activity and be cardioprotective in experimental ischemic animal models; the extracts decreased myocardial oxygen consumption and left ventricular work . Prophylactic antiarrhythmic potential has also been shown in rabbits that received aconitine. Mild CNS depressant effects have been documented for the hawthorn flower extract.

Reported Uses

Claims for hawthorn surround its use in arteriosclerosis, Buerger’s disease, heart failure, hypertension, and paroxysmal tachycardia. It may be therapeutically useful in the treatment of New York Heart Association (NYHA) functional class II (mild to moderate) heart failure. Patients with this class of heart failure who received a daily dose of 600 mg of hawthorn extract showed significant clinical improvement over an 8­week period .

Hawthorn, either alone or with coenzyme Q10, was found to be beneficial and also compared favorably to captopril for patients with heart failure. Other studies have noted the herb’s usefulness in patients with stable angina pectoris .

Dosage

A dose of 160 to 900 mg of a standardized extract containing 2.2% flavonoids or 18.75% oligomeric procyanidines given P.O. b.i.d. or t.i.d. The amount of flavonoid (calculated as hyperoside) is 3.5 to 19.8 mg and that of procyanidins (as epicatechin) is 30 to 168.7 mg.

Adverse Reactions

CNS: fatigue, sedation (with high doses).

CV: arrhythmias and hypotension (with high doses).

GI: nausea.

Respiratory: respiratory failure (in animals).

Skin: sweating.

Interactions

Antihypertensives, nitrates: Increased risk of hypotension. Monitor blood pressure closely.

Cardiac glycosides: Increased effects of these drugs. Use cautiously.

CNS depressants: May cause additive effects. Use cautiously.

Contraindications and precautions

Hawthorn is contraindicated in patients who are hypersensitive to other members of the Rosaceae family and in pregnant or breast-feeding patients.

Special considerations

Monitor the patient for adverse CNS effects.

Instruct the patient to use hawthorn only under medical supervision.

Caution the patient to avoid hazardous activities until hawthorn’s CNS effects are known.

Inform the patient that other proven therapies for heart failure should be pursued before taking hawthorn.

Urge the patient to seek emergency medical treatment if he becomes short of breath or if pain occurs in the heart region and spreads to the arm, lower jaw, or upper abdomen.

Urge the patient who chooses to self-medicate to seek medical advice if symptoms continue for longer than 6 weeks.

Points of Interest

Germany’s Federal Institute for Drugs and Medical Devices has approved the use of hawthorn leaf with flower extracts in the treatment of NYHA functional class II heart failure. The extract of berries has not been approved because efficacy has not been shown.

Berry preparations are commonly advertised as a supplement to strengthen and invigorate the heart and circulatory system.

Commentary

Hawthorn has long been used for heart failure in Europe. Several foreign studies suggest that it may be effective in treating NYHA functional class II heart failure. Long-term studies using hawthorn that demonstrate prolonged survival are lacking. Future studies should focus on evaluating improvements in NYHA heart failure class, hospital admission rates, quality of life measurements, and whether hawthorn extracts have an effect on mortality.

Taxonomic Class

Rutaceae

Common Trade Names

Multi-ingredient preparations: Jaborandi, Origin Hair and Scalp Therapy, Wonder Gel, X-Tablets

Common Corms

The leaves from the jaborandi tree are available as essential oil, fluidextract, a powder, and tincture. Combination products are found as gels and tablets. Pilocarpine, the main active ingredient, is available in many prescription products:

Ocular insert: 20 mcg, 40 mcg

Ophthalmic gel: 4%

Ophthalmic solution: 0.25%, 0.5%, 1 %,2%,3%,4%,5%,6%,8%, 10%

Tablets: 5 mg

Source

Pilocarpus, or jaborandi, consists of the leaves of Pilocarpus jaborandi (Pernambuco jaborandi), Pilocarpus microphyllus (Maranham jaborandi), or Pilocarpus pinnatifolius (Paraguay jaborandi). The plant is native to the northern and northeastern parts of Brazil.

Chemical Components

Three alkaloids are found in jaborandi: pilocarpine, pilocarpidine, and isopilocarpine. Also reported are jaborine, pilosine, volatile oils (including dipentene), and jaboric, pilocarpic, and tannic acids.

Actions

When applied topically to the eye, pilocarpine stimulates muscarinic receptors; this causes the pupil to constrict and the ciliary body to contract, thus improving the outflow of aqueous humor. Muscarinic alkaloids, when administered orally, stimulate the smooth muscles of the GI tract, increasing motility and tone. The tone and motility of other organs or organ systems (such as the ureter, bladder, gallbladder, and biliary ducts) may also be increased. Pilocarpine causes increased sweating and salivation in humans. It acts on the CV and respiratory systems as well (decreases blood pressure, heart rate, and vital capacity). In cats, pilocarpine has caused cortical stimulation .

Jaborine, a component found in the leaves, may actually be antagonistic to pilocarpine. Tannic acid has local astringent properties that act on the GI mucosa and has shown anti ulcerative and antisecretory effects within the GI tract.

Reported Uses

Although jaborandi has several reported uses, pilocarpine is usually extracted and used to stimulate saliva secretion or as a diaphoretic or myotic . Pilocarpine is primarily used to treat glaucoma or xerostomia. Other reported uses of the jaborandi plant include treatment of Bright’s disease, deafness, diabetes, edema, intestinal atony, jaundice, nausea, nephritis, pleurisy, psoriasis, rheumatism, syphilis, and tonsillitis. A decoction of the leaf applied locally has been used as a treatment for baldness.

Dosage

For glaucoma, 1 or 2 gtt applied t.i.d. or q.i.d. Refer to package insert for pilocarpine for specific dosing information.

For xerostomia, 15 to 30 mg P.O. daily; a dose of 100 mg P.O. is considered fatal.

The following daily doses have been suggested: powdered leaves, 5 to 60 grains (0.324 to 3.9 g); fluidextract, 10 to 30 gtt; tincture, Y, to 1 dram (1.75 to 3 ml).

Adverse Reactions

CNS: headache.

CV: bradycardia.

EENT: increased salivation, lacrimation, visual changes.

GI: nausea, vomiting.

Skin: sweating.

Interactions

Anticholinergics (atropine, ipratropium, scopolamine, other belladonna­type alkaloids): May decrease effects of these drugs. Avoid administration with jaborandi.

Beta blockers: May cause conduction problems. Monitor the patient.

Glycosides, iron-containing compounds, other alkaloids: Tannic acid may interact with these drugs. Do not use together.

Other prescription products containing pilocarpine, other muscarinic agonists (arecoline, methacholine, muscarine), cholinesterase inhibitors (do­nepezil, edrophonium, physostigmine): May have additive effect when used concomitantly. Use cautiously to avoid toxicity.

Contraindications And Precautions

Jaborandi is contraindicated in patients who are hypersensitive to pilocarpine and in those with uncontrolled asthma, acute iritis, and angleclosure glaucoma. Avoid use in pregnant or breast-feeding patients. Avoid large doses of jaborandi because hepatic injury can occur, especially in patients with preexisting hepatic disease. Use cautiously in patients with significant CV disease, biliary tract or urogenital abnormalities (cholelithiasis, nephrolithiasis), and preexisting cognitive or psychiatric disorders.

Special Considerations

Monitor intraocular pressure in patients at risk for glaucoma.

Monitor liver transaminase levels; if they increase, the product should be discontinued immediately.

Inform the patient that excessive sweating may lead to dehydration if fluids are not replenished.

Alert Signs of pilocarpine toxicity include exaggerated muscarinic effects. Extreme cases may lead to severe bronchospasm, hypotension, pulmonary edema, and shock. Treatment consists of atropine administration and general support of the CV and respiratory systems to counteract the effects from pulmonary edema .

Urge the patient to immediately report symptoms associated with pilocarpine toxicity (excessive sweating, lacrimation, increased salivation, nausea, vomiting, hypotension, and bradycardia) or hepatic dysfunction (fever, jaundice, and pain in right upper quadrant). Instruct him to discontinue use of the product if they occur.

Caution the patient that pilocarpine may cause visual changes, especiallyat night, which may impair his ability to drive.

Advise the pregnant or breast-feeding patient not to use jaborandi.

Commentary

The jaborandi tree is regarded as a source for pilocarpine. Much information exists about the use of pilocarpine for treating glaucoma and xerostomia. No human studies are available that support the use of jaborandi leaves for any medicinal purpose. Patients with glaucoma, xerostomia, or other potentially treatable conditions should seek medical advice because self-medication with jaborandi is not advised.